Paclitaxel and Erlotinib-co-loaded Solid Lipid Core Nanocapsules: Assessment of Physicochemical Characteristics and Cytotoxicity in Non-small Cell Lung Cancer
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Lung cancer is the leading cause of cancer-related deaths. The aim of this study was to design solid lipid core nanocapsules (SLCN) comprising a solid lipid core and a PEGylated polymeric corona for paclitaxel (PTX) and erlotinib (ERL) co-delivery to non-small cell lung cancer (NSCLC), and evaluate their physicochemical characteristics and in vitro activity in NCI-H23 cells.
PTX/ERL-SLCN were prepared by nanoprecipitation and sonication and physicochemically characterized by dynamic light scattering, transmission electron microscopy, differential scanning calorimetry, X-ray diffraction, and Fourier-transform infrared spectroscopy. In vitro release profiles at pH 7.4 and pH 5.0 were studied and analyzed. In vitro cytotoxicity and cellular uptake and apoptosis assays were performed in NCI-H23 cells.
PTX/ERL-SLCN exhibited appropriately-sized spherical particles with a high payload. Both PTX and ERL showed pH-dependent and sustained release in vitro profiles. PTX/ERL-SLCN demonstrated concentration- and time-dependent uptake by NCI-H23 cells and caused dose-dependent cytotoxicity in the cells, which was remarkably greater than that of not only the free individual drugs but also the free drug cocktail. Moreover, well-defined early and late apoptosis were observed with clearly visible signs of apoptotic nuclei.
PTX/ERL-SLCN could be employed as an optimal approach for combination chemotherapy of NSCLC.
Key WordsErlotinib paclitaxel solid lipid core nanocapsules non-small cell lung cancer
Acetate buffer solution
Dynamic light scattering
Dulbecco’s Modified Eagle’s medium
Differential scanning calorimetry
Epidermal growth factor receptor
Fluorescence-activated cell sorting
Fetal bovine serum
Fourier-transform infrared spectroscopy
High-performance liquid chromatography
Molecular weight cut-off
Non-small cell lung cancer
Small cell lung cancer
Solid lipid core nanocapsules
Transmission electron microscopy
Tyrosine kinase inhibitor
Acknowledgments and Disclosures
This research was supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MSIP) (No. 2015R1A2A2A01004118, 2015R1A2A2A04004806, and by the Medical Research Center Program (2015R1A5A2009124) through the NRF funded by MSIP).
Compliance with Ethical Standards
Conflict of Interest
The authors have no conflict of interest to declare.
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